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Transgender

Our Transgender category contains feminizing products including female hormones and male hormone antagonists for transgender hormone therapy, and also for reducing facial hair for male-to-female transsexuals.

The different classes of Transgender medication are listed on the left of the page and when you click on one of these, the principal brand name products display in the left column and generic alternatives to the right.

Use the search feature to quickly find the product you are looking for, by entering either the active ingredient, e.g. Dutasteride, or the product name, e.g. Duprost

Our Anti-Androgens class of Transgender products contain products that are used to block the actions of testosterone and reduce the effects of male hormones during a gender reassignment programme. 

Use the search feature to quickly find the product you are looking for, by entering either the active ingredient, e.g. Flutamide, or the product name, e.g. Cytomid. 

What is an androgen?

Androgen is a generic term for male hormones which are steroid hormones that bind to the androgen receptor and control the development of male characteristics.  The main androgen is testosterone, which is converted to its active and more potent metabolite dihydrotestosterone (DHT) by the action of the enzyme 5-alpha reductase and.  Both testosterone and DHT bind to the androgen receptor within responsive cells of various tissues including brain, bone, hair follicles, testes and prostate cells.  

What is an anti-androgen?

Anti-androgens are drugs that counteract or block the biological effects of the male hormone testosterone or its active metabolite DHT on a wide range of tissues where they normally have biological activity.  They are usually steroidal and fat soluble and pass through the cell membrane to interact with the androgen steroid receptors inside the cell and compete with testosterone or DHT for these receptors.  This blocks expression of genes involved in the development and maintenance of male characteristics. 

Some anti-androgens are non-steroidal and also compete with testosterone and DHT for receptor binding, thereby blocking the action of testosterone and also the production of testosterone by the testes.  Other non-steroidal anti-androgens inhibit the conversion of DHT from testosterone.  Some drugs have anti-androgenic activity as a side effect. 

Products for blocking the action of androgens

  • Dutasteride and Finasteride are 5α-reductase inhibitors and work by inhibiting the action of the enzyme type II 5α-reductase, which converts the male hormone testosterone to DHT
  • Flutamide is a non-steroidal anti-androgen that blocks the action of androgens by binding to same receptor but has no steroid effects
  • Bicalutamide is a non-steroidal anti-androgen
  • Cyproterone is a steroidal anti-androgen
  • Spironolactone is a synthetic steroid which is primarily a diuretic but has anti-androgenic activity as a side effect and works by by decreasing androgen production 
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Our Estrogens class of Transgender products contain various forms of the female hormone estrogen for use in a feminizing regime for transgender hormone therapy during a gender reassignment programme. 

Use the search feature to quickly find the product you are looking for, by entering either the active ingredient, e.g. oestradiol, or the product name, e.g. Climara.

About estrogen

Estrogens are produced by the ovaries along with progesterone at certain stages of the menstrual cycle and their production is under control of follicle stimulating hormone (FSH) and luteunising hormone (LH) produced by the pituitary gland, which are in turn under the control of gonadotrophin releasing hormones produced by the hypothalamus in the brain.  

Estrogen is the main female hormone that stimulates development of female secondary sexual characteristics like breast development, body shape and regulating the menstrual cycle.  Therefore, estrogen is used as the main component of trangender hormone therapy for male to female transexuals while at the same time overriding the effects of testosterone.  

Different forms of estrogen

Estrogen exists in several forms and with different potencies:

  • Estradiol, specifically 17-beta-estradiol or E2, is the major and most active form of natural estrogen in the body produced by the ovaries and is responsible for the main actions of estrogen
  • Ethinyloestradiol is a synthetic form of 17-beta-estradiol that is more resistant to metabolism in the liver than natural estradiol but has the same biological activity. 
  • oestradiol valerate is a prodrug (or precursor) of natural human oestradiol and is converted to 17-beta-estradiol by esterase enzymes in the blood and liver.  It is an effective form of estrogen used for intramuscular administration (injection) as it is absorbed slowly and lasts longer that estradiol itself. 
  • Estrone or E1 becomes the most prominent form of natural estrogen during menopause, as estradiol drops, and is produced primarily in the adrenal glands.  Estrone is readily converted into a long lasting form estrone sulphate which concentrates in breast tissue of post-menopausal women and is thought to be involved the development of breast cancer, by being converted to estradiol.  
  • Estriol or E3 is the weakest of the three natural forms of oestrogen.  It is the prominent form of estogen during pregnancy and is produced by the placenta, but plays no significant role in non-pregnant women as it is mild, short acting and normally present in small amounts.
  • Conjugated oestrogens are a mixture of several different forms of estrogen (at least 10) isolated from horse urine.  They contain mainly forms of estrogen that are in the sulphate form and can be easily absorbed and converted to the active form estradiol.

Delivery methods for estrogens

Estrogen hormone replacement therapy is available in several different preparations and routes of administration.  These include:

  • Oral preparations which are subjected to metabolism by the liver and is associated with side effects, such as painful swollen breasts, nausea, headache.
  • Skin patches allow oestrogen to diffuse through the skin and into the blood and allows for lower doses to be used, as estrogen bypasses liver and is therefore, not subject to first pass metabolism by the liver.  It also provides more constant blood levels as it diffuses into the blood at a steady rate
  • Topical transdermal creams and gels which are rubbed into the skin so that the estrogen diffused through the skin directly into the blood circulation, allowing the estrogen to be released slowly through the skin. 

Products available for estrogen hormonal therapy

The most commonly used estrogens as part of a feminising regime for transgender hormone therapy are the more potent forms of estrogen including estradiol (17-beta-estradiol), oestradiol valerate and conjugated oestrogens.  Estriol can also be used but is less effective.

  • estradiol for oral administration, skin patch or injection
  • oestriol for oral administration
  • conjugated oestrogens for oral administration
  • oestradiol valerate for injection
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Our Facial Hair Reduction class of Transgender products contains a product for removing unwanted facial hair for use in a feminizing regime during a male to female gender reassignment programme. 

Use the search feature to quickly find the product you are looking for, by entering either the active ingredient, e.g. eflornithine, or the product name, e.g. Eflora. 

Hormonal control of hair development

Androgen hormones are responsible for secondary sexual characteristics in men, including facial hair growth.  Androgens regulate the hair follicles and at puberty transform them from vellus follicles that produce the tiny almost invisible hairs that cover both male the and female body into the larger terminal follicles, producing pigmented hairs typical of the male facial hair, as well as chest hair and other body hair.  Androgens, particularly the active metabolite of testosterone dihydrotestosterone (DHT) also inhibit hair in other parts of the body, such as on the scalp by causing the terminal follicles to regress to vellus follicles, causing male pattern baldness or androgenic alopecia.

Use of anti-androgens as part of a feminising regime will reduce the amount and type facial hair, but may not eliminate it altogether.  

The hair growth cycle and its regulation

Hair goes through a 3-stage growth cycle.  The anagen phase, which is the active growth phase, catagen, where the hair stops growing and shrinks, before being shed during the telogen phase, to be replaced by a new hair.

The enzyme ornithine decarboxylase is an important rate limiting enzyme required the biosynthesis of certain proteins required for hair growth and is found in high levels in the hair follicles during the anagen phase of the hair growth cycle.  The levels of this enzyme then drop as the hair follicle enters the catagen phase.  Ornithine decarboxylase is also important in cell division and cell proliferation and actively growing hairs undergo rapid cell division. 

Blocking hair growth

Eflornithine is a drug that binds to ornithine decarboxylase and inhibits its activity. This action of ornithine decarboxylase can be used to block the growth and cell division of the terminal hair follicles that produce facial hair.  It is available as a topical cream and can help slow down the production of facial hair during the feminisation programme but it does not destroy the hair or prevent it from growing back.  
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Our Progestins class of Transgender products contain various forms of the female hormone origesterone, as progestins and progestogens for use in a feminizing regime for transgender hormone therapy during a gender reassignment programme. 

Use the search feature to quickly find the product you are looking for, by entering either the active ingredient, e.g. medroxyprogesterone, or the product name, e.g. Depo Provera.

What are progestins and progestogens?

Progesterone is the female hormone that in women prepares the endometrium (lining of the uterus) for a potential pregnancy.  Progestogens have the same biological activity as naturally occurring progesterone but the chemical structure has been slightly altered to improve stability and absorption. Progestins are synthetic progestogens that have a different chemical structure to progesterone but similar biological effects. 

Progestins and progestogens are used medically for contraception, hormone replacement therapy in menopausal women and to treat certain conditions like endometriosis.  

Use of progestins and progestogens for transgender hormone therapy

Although the clinical opinion is mixed on their effectiveness of use, progestins and progestogens can be used as part of the feminization regime for male to female transgender hormone therapy1.  The rational for this is that adding progesterone in some form more closely simulates the female hormone cycle.  However, there are also some side effects including, weight gain, oedema, and mood swings.  There is also an increased risk of developing breast cancer2.

Progesterone suppresses testosterone production and is also thought to support breast development in transgender hormone therapy, which is one of the roles of progesterone in females.  Although oestrogen is primarily responsible for breast development in females, progesterone is involved in regulation the growth and differentiation of breast tissue.  Also during pregnancy, progesterone contributes to increasing the size of breasts and the nipples in preparation for lactation. 

Progestin products

Progestins, which are synthetic progestogens, available are:

  • Medroxyprogesterone
  • Hydroxyprogesterone
  • Dydrogesterone
Medroxyprogesterone and hydroxyprogesterone are both administered by injection and are more potent and longer-acting than natural progesterone. Medroxyprogesterone is also available for oral administration as is dydrogesterone.  Progestins are more active when taken orally than natural progesterone and do not have other hormonal effects.

Progestogen products

Micronized progesterone, in which natural progesterone is reduced to tiny particles for better absorption, is available as a gel and as capsules.

Progesterone is also available for injection in an oil base for stability. 

References

  1. Wierckx K, Gooren L, T'Sjoen G. Clinical review: Breast development in trans women receiving cross-sex hormones. J Sex Med 2014 May;11(5):1240-7
  2. Axlund SD, Sartorius CA. Progesterone regulation of stem and progenitor cells in normal and malignant breast. Mol Cell Endocrinol 2012 Jun 24;357(1-2):71-9. 



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Our Transgender – Others sub-category medications contain cost-effective branded medicines and generic alternatives.  These products support the transgender process for patients undergoing both male to female, and female to male gender reassignment.

You can search for the product you want using the search box, by entering either the active ingredient, e.g. Cyproterone or the product name, e.g. Climen.

Anti-oestrogens

Anti-oestrogen medicines, such as tamoxifen and anastrozole, are used to treat breast cancer in women.  They can also be used to support the gender reassignment process for female to male transgender patients.  Anastrozole blocks the synthesis of oestrogen in peripheral tissues such as adrenal glands and fat tissue, where testosterone can be converted to oestrogen.  Tamoxifen blocks activation of the oestrogen receptor, preventing stimulation of female secondary sexual characteristics like breast tissue.  Both medications help reduce the amount of oestrogen, which supports the suppression of female characteristics and the increase in masculine characteristics.

Combination products

Combining medications that promote female characteristics while suppressing male characteristics, can help with the male to female gender reassignment process.

Medications combining oestrogen with an antiandrogen like cyproterone, are used to treat conditions in women caused by overproduction of androgens.  These conditions include hirsutism (unwanted hair) and acne.  Cyproterone alone is used to control extreme sexual desire in men that can cause aggressive behaviour.  A combination of oestrogen with an antiandrogen can also be used to promote feminization while suppressing male characteristics, which helps support the gender reassignment process for male to female transgender patients.  Oestrogens promote female characteristics, such as stimulating breast development and help make changes to the male body, such as reducing muscle mass and redistributing body fat.  Antiandrogens are drugs that block the production and the effects of the male hormone testosterone and its more potent form, dihydrotestosterone (DHT).  Development of secondary male characteristics are stimulated by DHT.  These include growth of the prostate gland, the testes, and body and facial hair. 

Several forms of oestrogen can be used to promote the feminization process.  These include conjugated oestrogens, which is a mixture of natural oestrogen in different forms.  This preparation of oestrogen is used for hormone replacement therapy in women, to relieve symptoms of menopause.  Conjugated oestrogens can also be used for hormone therapy as part of the gender reassignment process in male to female patients.  Oestrogen combined with a progestogen like medroxyprogesterone, a synthetic form of the female sex hormone progesterone, may enhance the feminization process.  Progesterone is involved in breast development.  It also has antiandrogenic activity and works by blocking testosterone production.

Topical anaesthetic cream

A cream containing a combination of two topical anaesthetics is used for pain relief during minor superficial surgical procedures.  These types of surgery may be needed during the gender reassignment process, for example, surgery involving genital skin.

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A gender reassignment program for male to female transsexuals normally includes reducing androgen effects with spironolactone (cyproterone has been used in European countries) and stimulating feminization of secondary sex characteristics with estrogen.
There can be risks attached to hormone therapy in both men and women and therefore it is definitely inadvisable to take any form of hormone product unless it is medically prescribed.
The use of progesterone to augment breast development is controversial in physicians treating MTF transsexuals. When deciding on a hormone regimen, prescribers should remember that it is estrogen that causes the serious side effects, so the lowest effective dose should be used.
The manufacturers of oestrogen and progesterone products specify them for medical use in females and do not acknowledge their use for transsexuals, so there is little clinical data available regarding this usage.
Apart from a summary provided below, two excellent sites for information on hormones and dosages are:
http://www.scribd.com/doc/56618709/transsexual-transgendered-guide-to-obtaining-and-using-transsexual-hormones-hormone-replacement-therapy-hrt

Estrogens

Estrogen dosing regimens for gender transition vary widely. Estrogen should be prescribed at the lowest possible effective doses to avoid the serious complications of high-dose estrogen therapy.
Current recommendations for estrogen dosing range from starting doses of 0.625 to 2.5 mg of conjugated estrogen.
Estrogen is the most important part of any feminizing regimen.

Some typically-used estrogen dosages for pre-operative transsexual women who have not had an orchiectomy (castration) are as follows:

Oral Estrogens

Conjugated estrogens such as Premarin® 5 mg daily.
Estradiol such as Progynova (Oestradiol Valerate) or Estrofem 4 mg daily.

Injectable Estrogen

Progynon Depot is an alternative form of Oestradiol Valerate and comes in an injectable form.

Transdermal Estrogen

Estradiol 0.1 mg patch, changed twice weekly. Transdermal patches uniformly contain estradiol as the active medication, produced in 0.05mg (50 mcg), 0.075mg (75 mcg) and 0.1 mg (100 mcg) concentrations, and are branded under a variety of names such as Estradot / Vivelle, Climara and Estraderm.
Transdermal estrogen causes less clotting tendency than oral estrogen, possibly important to some patients; but this is a very expensive product.

Estrogen Gels

If you do not wish to use estradiol patches, an option is estradiol gel applied daily to the skin. The gel is usually alcohol based and is absorbed through the skin. The medication imparted into the skin usually takes about 12 hours for absorption into the blood stream, which produces a similar continuous action like the patch. Gels have the advantage as the wearer is not burdened with wearing a patch and the potential irritation from the adhesive that holds the patch in place.
Gels roughly corresponds to the daily doses found in the 50 mcg and 100 mcg patches.
Sandrena is an Estradiol Gel which comes in 1 gram sachets.
Estrodose Gel is the same as Estrogel. It is a clear, odorless, hydro-alcoholic gel that provides for delivery of estradiol for estrogen replacement in a non-patch transdermal form.

Other Forms of Estrogen

InhousePharmacy.vu is able to provide three other forms of Estrogen these are Premarin Cream which is a conjugated Estrogen Cream and Ovestin which is a low dose Estriol Cream.
Aerodiol - Aerodiol nasal spray containing estradiol hemihydrate 150µg per spray has been launched by Servier Laboratories The product is licensed for replacement therapy for oestrogen deficiency symptoms in postmenopausal women.
Serious health risks of estrogen therapy include stroke, pulmonary embolism, myocardial infarction, and breast cancer.

Combination estrogen and progesterone

InhousePharmacy.vu is able to supply Kliogest and Kliovance / Activelle, a combination of oestradiol and norethisterone and is used to produce female hormones estrogen and progesterone.

Antiandrogens

Besides providing estrogen, a hormone regimen should also reduce testosterone to normal female levels. This usually requires adding an anti-androgen.
Spironolactone acts as an antiandrogen of testosterone to dihydrotestosterone. Spironolactone in doses of 200–400 mg per day allows the practitioner to decrease exogenous estrogen doses tophysiologic or “hormone replacement” levels while still obtaining desired effects of breast development, feminization of skin, and female fat distribution.
Spironolactone can usually be discontinued after sex reassignment surgery.
Androcur (Cyproterone acetate) is a powerful antiandrogen and progestagen used in Europe for transgendered patients. Its use is limited by interference with corticosteroid production, high cost, and side effect profile.
Cyproterone is a generic form of Androcur. It performs is exactly same way as Androcur but at a cheaper cost.
Finasteride is an antiandrogen that opposes the formation of DHT, but not of testosterone itself. Finasteride is present in Proscar in a 5mg dosage and in Propecia in a 1mg doasge.
Dutasteride is also an antiandrogen that opposes the formation of DHT, but not of testosterone itself.
There are several other antiandrogens which are used for other indications but have no reported data in the transgendered patient. Flutamide and Bicalutamide are nonsteroidal antiandrogens normally used in the management of Management of Prostate Cancer.

Progesterone

Progesterone is the third and optional component of the MTF regimen.
Medroxyprogesterone is available as Provera and Depo-Provera. Medroxyprogesterone is a weak antiandrogen, and testosterone suppression may be accomplished with lower doses of estrogen. Medroxyprogesterone is less androgenic than norethindrone and orgestrel.
Micronized Progesterone is advantageous because it has a more favorable side effect profile (anxiety and irritability) than medroxyprogesterone. It is also less androgenic when higher progesterone doses are needed, but is more costly. Micronized progesterone is available as Prometrium or in a generic form as Microgest.
Duphaston (Dydrogesterone) may be used as an alternative to medroxyprogesterone acetate. It is not metabolised into testosterone within the body, and is therefore free of the virilising effects which some patients experience ftom other progesterones. A typical pre-op (or early post-op) dose would be 20mg in two doses, reducing to a single dose of 10mg daily post-op.
Crinone is another medication available and contains the female hormone progesterone.
Cyproterone plus Estrogen
While Androcur is available in 50 mg tablets, sometimes Diane-35 is used when small doses are desired. Diane-35 is a contraceptive with anti-acne properties (due to the cyproterone contained), and is comprised of 2 mg of cyproterone acetate and 0.035 mg ethinyl estradiol. Diane-35 generics are available.
InhousePharmacy.vu can supply Diane 35 which is comprised of 2 mg of cyproterone acetate and 0.035 mg ethinyl estradiol.
A generic form of Diane 35 is also available, this is manufactured by Cipla and is known as Ginette 35.
Climen is also a combination of an Estrogen with Cyproterone. Climen is normally used in Hormone Replacement Therapy Calendar-pack containing 11 tablets of 2 mg estradiol-17-valerate each, plus 10 tablets of 2 mg estradiol-17-valerate and 1 mg cyproterone acetate each. Brandnames in other countries - Climene, Climen/Clisin.

Facial Hair Reduction

Eflora / Vaniqa Cream is used for the reduction of unwanted facial hair. Eflora / Vaniqa Cream does not remove hair, it slows the regrowth.

Antagonists

Anastrozole is a non-steroidal aromatase inhibitor that decreases the amount of estrogen the body makes.
Arimidex contains the active ingredient anastrozole to decrease the body's production of estrogen.
InhousePharmacy.vu are unable to provide advice on treatment regimes. However the following sites may be of some assistance.

Transsexual Women's Resources

TransGenderCare - An educational offering of the Tampa Gender Identity Program. Has useful features on hormones and medical care.
http://www.transgendercare.com
and another excellent site is
http://www.scribd.com/doc/56618709/transsexual-transgendered-guide-to-obtaining-and-using-transsexual-hormones-hormone-replacement-therapy-hrt

Read more

What is gender?

Gender is a word that encompasses ways of differentiating male and female or masculine and feminine.   However, gender is not an easy word to define, as there are many components to its definition, which generally includes behaviour patterns, activities, social identity and psychological traits that are considered by a society or culture as typically associated with one sex, male or female, as well as biology and genetics.  

In 1955 gender was first described in terms of sexual roles by John Money, a doctor specialising in research into the biology and psychology of gender.  He also used the term gender identity for the first time in 1966 to describe a person’s subjective sense of their own sex, which may not be the same as their physical gender based on the genitals they were born with. 

In 1974 the term gender dysphoria was first used to describe the distress that can be felt by a person who is dissatisfied or discontented with the physical sexual identity they were born with or the sexual role in society that is expected of them and this is also known as gender identity disorder.  This therefore, describes people who have a gender identity that does not match their physical gender and includes people described by the categories of transsexual or transgender.

Transgender or transsexual

A transgenderist describes a person who lives within their body and is not necessarily male or female, but may incorporate both male and female behaviour and appearance.  They usually do not wish to have genital surgery and manage their gender identity by the way they dress and how they present themselves. 

A transsexual is someone who has a gender identity that more closely resembles the opposite sex and they often wish to change their physical sex attributes and live completely as the opposite sex.  For a transsexual the next step would be genital surgery and hormone therapy to complete the gender reassignment process.  

Gender reassignment

The term gender reassignment refers to the process whereby the physical sexual characteristics are altered to reflect a person’s gender identity.  This process of change from the one gender to another, also known as transition, incorporates medical procedures, hormone replacement therapy and social changes, such as the person’s role and legally changing their name to one that better suits the opposite gender. 

The genetics of gender 

Gender is determined by several factors, including hormones present during foetal development, reinforced behaviour patterns as well as genetics.  While genetics usually determines gender, XX being female and XY being male, there are other genetic combinations that introduce shades of grey.  Some of these change the physical appearance, such as XXY, which results in male and female genitals and is known as Klinefelder’s syndrome.  The genetic makeup XYY results in male genitals but can also cause various antisocial or aggressive behaviours.  The genetic makeup XO or Turner’s syndrome results in a female body but behaviour and personality are affected.   

The role of hormones in sex and gender

The term sex refers to the biological difference between the male and female body.  However, gender refers to the expected behavioural and cultural differences within society that is determined by a person’s sex.  Without intervention a person’s sex does not change but gender can. 

The physical differences between males and females develop in response to steroid hormones and these begin influencing development before birth.  All foetuses develop along female lines until testicular hormones initiate male differentiation.  Although oestrogen is considered the female hormone, testosterone is also present in females but in lesser amounts and it is the higher levels of testosterone in males that determines the development of male physical changes and also influences brain development, which ultimately influences behaviour.  

At puberty female secondary sexual characteristics are induced by oestrogen and progesterone produced by the ovaries and male secondary sexual characteristics are induced by androgens, particularly testosterone and its potent metabolite dihydrotestosterone or DHT produced by the testes.  

Feminization regime

Gender reassignment hormone therapy for male to female transsexuals is based on suppressing the original male characteristics by blocking male hormones and stimulating development of female secondary sexual characteristics using female hormones.  This process is known as a feminizing programme and several hormones are available to help with this process.  Removal of body and facial hair are also part of the feminizing process. 

The effects of male-to-female hormonal therapy include redistribution of body fat to redefine body shape; breast development, reduction in appearance and coarseness of body hair; reduced musculature in the hands and feet; changes in appearance of the skin and reduced activity of the sebaceous glands.  

Products for feminisation hormone therapy

Feminizing hormone therapy comprises the following drug regimen:

  • Estrogens the female hormone that exists in different forms, the most potent in promoting female characteristics is estradiol.  Estrogens can be used for oral, transdermal (patches, creams and gels) and injectable administration. 
  • Anti-androgens reduce the effects of the male hormone testosterone
  • Progestins, derived from naturally occurring progesterone, is a hormone that is found in both males and females and can help promote the feminisation process.
  • Combination estrogen and progesterones, where the progesterone component may help counteract some of the risks of estrogen alone. 
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